.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

DrugPatentWatch Database Preview

Claims for Patent: 4,517,199

« Back to Dashboard

Claims for Patent: 4,517,199

Title: Method for lowering intraocular pressure using phenylimino-imidazoles
Abstract:2-(Trisubstituted phenylimino)-imidazole compounds also known as 2-(trisubstituted anilino)-1,3 diazacyclopentene-(2) compounds are used to lower intraocular pressure.
Inventor(s): York, Jr.; Billie M. (Fort Worth, TX)
Assignee: Alcon Laboratories, Inc. (Fort Worth, TX)
Application Number:06/519,791
Patent Claims: 1. A method for lowering intraocular pressure comprising topically applying to the eye an effective amount for lowering such intraocular pressure of a 2-(trisubstituted phenylimino)-imidazoline, or a pharmaceutically acceptable salt thereof, having the formula ##STR64## where R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are defined in accordance with either I, II, or III as follows:

I. R.sub.1 =R.sub.2 =methyl, ethyl, trifluoromethyl, chloro or bromo.

R.sub.1 .noteq.R.sub.2 and each=methyl, ethyl, trifluoromethyl, fluoro, chloro and bromo,

one of R.sub.3 and R.sub.4 is H and the other is selected from ##STR65## R.sub.5 .noteq.R.sub.6 =H or lower alkyl, R.sub.5 =R.sub.6 and each=H, lower alkyl,

R.sub.7 =H, lower alkyl 2-hydroxyethyl, 2-hydroxypropyl or 3-hydroxypropyl,

the sum of the carbon atoms in R.sub.5 and R.sub.6 or R.sub.5 and R.sub.7 being 4 or less, or ##STR66## R.sub.8 =lower alkyl; II. R.sub.1 =methyl, ethyl, trifluoromethyl, chloro or bromo,

R.sub.2 =H,

R.sub.3 =is selected from ##STR67## R.sub.4 =methyl, chloro or bromo R.sub.9 =H or lower alkyl,

R.sub.10 =H, lower alkyl, 2-hydroxymethyl, 2-hydroxypropyl or 3-hydroxypropyl,

the sum of the carbon atoms in R.sub.9 and R.sub.10 being 4 or less;

III. In no event shall said 2-(trisubstituted phenylimino)-imidazoline have the formula: ##STR68##

2. A method in accordance with claim 1 wherein the 2-(trisubstituted phenylimino)-imidazoline or salt is topically applied to the eye in a pharmaceutically acceptable vehicle.

3. A method in accordance with claim 2 wherein the concentration of the 2-(trisubstituted phenylimino)-imidazoline or salt is selected such that intraocular pressure is reduced without significantly affecting the central nervous system.

4. A method in accordance with claim 3 wherein the 2-(trisubstituted phenylimino)-imidazoline is 2,6-Dichloro-N.sup.1 -(2-imidazolidinylidene)-1,4-benzenediamine having the structure: ##STR69## or pharmaceutically acceptable salt thereof.

5. A method in accordance with claim 3 wherein the 2-(trisubstituted phenylimino)-imidazoline is 2,6-Dichloro-N.sup.1 -(2imidazolidinylidene)-1,3-benzenediamine having the structure: ##STR70##

or pharmaceutically acceptable salt thereof.

6. A method in accordance with claim 3 wherein the 2-(trisubstituted phenylimino)-imidazoline is 2,6-Diethyl-N.sup.1 -(2-imidazolidinylidene)-1,4-benzenediamine having the structure of: ##STR71## or pharmaceutically acceptable salt thereof.

7. A method in accordance with claim 3 wherein the 2-(trisubstituted phenylimino)-imidazoline is N-[3,5-Diethyl-4-(2-imidazolidinyleneamino)-phenyl]-acetamidne having the structure: ##STR72## or pharmaceutically acceptable salt thereof.

8. A method in accordance with claim 3 wherein the 2(trisubstituted phenylimino)-imidazoline is 3,5-Dichloro-4-(2-imidazolidinylideneamino)-phenol and esters thereof having the structure: ##STR73## or pharmaceutically acceptable salt thereof.

9. A method in accordance with claim 3 wherein the 2-(trisubstituted phenylimino)-imidazoline is 3-chloro-5-methyl-4-(2-imidazolidinylideneamino)-benzoic acid ethyl ester having the structure: ##STR74## or pharmaceutically acceptable salt thereof.

10. A method in accordance with claim 3 wherein the 2-(trisubstituted phenylimino)-imidazoline is 3-chloro-5-ethyl-4-(2-imidazolidinylideneamino)-benzoic acid ethyl ester having the structure: ##STR75## or pharmaceutically acceptable salt thereof.

11. A method in accordance with claim 3 wherein the 2-(trisubstituted phenylimino)-imidazoline is N-[3-chloro-5methyl-4-(2-imidazolidinylideneamino)-phenyl]-acetamide having the structure: ##STR76## or pharmaceutically acceptable salt thereof.

12. A method in accordance with claim 3 wherein the 2-(trisubstituted phenylimino)-imidazoline is 2 chloro-6methyl-N.sup.1 -(2-imidazolidinylidene)-1,4 benzenediamine having the structure: ##STR77## or pharmaceutically acceptable salt thereof.

13. A method in accordance with claim 3 wherein the 2-(trisubstituted phenylimino)-imidazoline is 2-chloro-6ethyl-N.sup.1 -(2-imidazolidinylidene)-1,4 benzenediamine having the structure: ##STR78## or pharmaceutically acceptable salt thereof.

14. A method in accordance wtih claim 3 wherein the 2-(trisubstituted phenylimino)-imidazoline is 3-chloro-5methyl-4-(2-imidazolidinylideneamino)-benzenecarboxamide having the structure: ##STR79## or pharmaceutically acceptable salt thereof.
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

`abc